GLPBio

SAG

Catalog No.: GC12068Purity:>99.50%Synonyms: Smoothened Agonist
COASDSData Sheet
SAG (Smoothened Agonist) is an effective Smo receptor agonist.

Products are for research use only. Not for human use. We do not sell to patients.

SAG
Cas No.: 912545-86-9
10mM (in 1mL DMSO)In Stock
$136.00
1
1mgIn Stock
$42.00
1
5mgIn Stock
$126.00
1
10mgIn Stock
$203.00
1
25mgIn Stock
$245.00
1
50mgIn Stock
$343.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

No citations are currently available for this product. Below are selected publications citing GlpBio products.
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

Description

SAG (Smoothened Agonist) is an effective Smo receptor agonist. SAG activates the Hedgehog signaling pathway. SAG induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3nM. In Cos-1 cells expressing Smo, SAG has a Kd of 59nM for the SAG/Smo complex[1-3].

SAG (250nM; 24h) promotes migration of MDA-MB-231 cells[4]. SAG(1μM; 6 days) treatment rescues mitochondrial dysfunction in FXN-deficient astrocytes[5].

SAG(15-20mg/kg；ip) generally induces preaxial polydactylism in a dose-dependent manner in mice[6]. SAG(20μg/g body weight; i.p; 3 times) restores Shh(Sonic hedgehog) signaling, leading to the rescue of BBB function in HIV-infected, humanized mice[7].

References:
[1]. Chen JK, Taipale J, et,al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6. doi: 10.1073/pnas.182542899. Epub 2002 Oct 21. PMID: 12391318; PMCID: PMC137838.
[2]. Bragina O, Sergejeva S, et,al. Smoothened agonist augments proliferation and survival of neural cells. Neurosci Lett. 2010 Sep 27;482(2):81-5. doi: 10.1016/j.neulet.2010.06.068. Epub 2010 Jul 1. PMID: 20600593.
[3]. Stanton BZ, Peng LF, et,al. A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol. 2009 Mar;5(3):154-6. doi: 10.1038/nchembio.142. Epub 2009 Jan 18. PMID: 19151731; PMCID: PMC2770933.
[4]. Guerrini G, Criscuoli M, et,al. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec;233(12):9799-9811. doi: 10.1002/jcp.26947. Epub 2018 Aug 21. PMID: 30132883.
[5]. Vicente-Acosta A, Giménez-Cassina A, et,al. The smoothened agonist SAG reduces mitochondrial dysfunction and neurotoxicity of frataxin-deficient astrocytes. J Neuroinflammation. 2022 Apr 12;19(1):93. doi: 10.1186/s12974-022-02442-w. PMID: 35413853; PMCID: PMC9006607.
[6]. Fish EW, Parnell SE et,al. Preaxial polydactyly following early gestational exposure to the smoothened agonist, SAG, in C57BL/6J mice. Birth Defects Res. 2017 Jan 20;109(1):49-54. doi: 10.1002/bdra.23571. PMID: 27801979; PMCID: PMC5388559.
[7]. Singh VB, Singh MV, et,al. Smoothened Agonist Reduces Human Immunodeficiency Virus Type-1-Induced Blood-Brain Barrier Breakdown in Humanized Mice. Sci Rep. 2016 May 31;6:26876. doi: 10.1038/srep26876. PMID: 27241024; PMCID: PMC4886511.

Protocol

Cell experiment [1]:

Cell lines

MDAMB 231 cells

Preparation Method

Cells were seeded at a concentration of 2 × 105 cells in 12 well/plates. When treated with compounds, cells were pretreated for 24h with SAG 250nM or DMSO as a control. The day after, a scratch was done using a p200 tip to the confluent monolayer; cells were then washed with PBS and resuspended in 1ml RPMI supplemented with 10% FBS and AraC (Cytosine β-D-arabinofuranoside; a selective inhibitor of DNA synthesis; 2.5µg/ml).

Reaction Conditions

250nM;24h

Applications

SAG promotes migration of MDA-MB-231 cells.

Animal experiment [2]:

Animal models

HIV-infected, humanized mice

Preparation Method

Mice were injected on alternate days with SAG (20μg/g body weight) or vehicle control, DMSO, for a total of 3 injections. Evans blue exclusion assay was performed to measure BBB permeability.

Dosage form

20μg/g body weight; i.p; 3 times

Applications

SAG rescues BBB(Blood Brain Barrier) integrity.

References:
[1]. Guerrini G, Criscuoli M, et,al. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec;233(12):9799-9811. doi: 10.1002/jcp.26947. Epub 2018 Aug 21. PMID: 30132883.
[2]. Singh VB, Singh MV, et,al. Smoothened Agonist Reduces Human Immunodeficiency Virus Type-1-Induced Blood-Brain Barrier Breakdown in Humanized Mice. Sci Rep. 2016 May 31;6:26876. doi: 10.1038/srep26876. PMID: 27241024; PMCID: PMC4886511.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
912545-86-9
Synonyms
Smoothened Agonist
Chemical Name
3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
SMILES
CN[C@@]1([H])CC[C@@](N(C(C2=C(Cl)C3=CC=CC=C3S2)=O)CC4=CC(C5=CC=NC=C5)=CC=C4)([H])CC1
Molecular Formula
C28H28ClN3OS
Molecular Weight
490.06
Solubility
≥ 24.5mg/mL in DMSO, ≥ 16.3mg/mL in Water with ultrasonic and warming
Storage
4°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

Reviews

Review for SAG

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%